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Literature summary extracted from

  • Shi, S.T.; Herlihy, K.J.; Graham, J.P.; Fuhrman, S.A.; Doan, C.; Parge, H.; Hickey, M.; Gao, J.; Yu, X.; Chau, F.; Gonzalez, J.; Li, H.; Lewis, C.; Patick, A.K.; Duggal, R.
    In vitro resistance study of AG-021541, a novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase (2008), Antimicrob. Agents Chemother., 52, 675-683.
    View publication on PubMedView publication on EuropePMC

Protein Variants

EC Number Protein Variants Comment Organism
2.7.7.48 I482S mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C
2.7.7.48 I482T mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C
2.7.7.48 M423I mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C
2.7.7.48 M423T mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C
2.7.7.48 M423V mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C
2.7.7.48 M426T mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C
2.7.7.48 V494A mutant confers resistance to AG-021541 and structurally related compounds but remains sensitive to interferon and HCV polymerase inhibitors known to interact with the active site or other allosteric sites of the protein Hepacivirus C

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.7.48 2-[2-chloro-4-(2-[2-cyclopentyl-5-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl]-4-hydroxy-6-oxo-3,6-dihydro-2H-pyran-2-yl]ethyl)phenyl]-2-methylpropanenitrile
-
 Hepacivirus C
2.7.7.48 2-[4-(2-[2-cyclopentyl-5-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl]-4-hydroxy-6-oxo-3,6-dihydro-2H-pyran-2-yl]ethyl)-2-fluorophenyl]-2-methylpropanenitrile
-
 Hepacivirus C
2.7.7.48 6-[2-(5-chloro-2,4-dimethoxyphenyl)ethyl]-6-cyclopentyl-3-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfanyl]-4-hydroxy-5,6-dihydro-2H-pyran-2-one AG-021541 Hepacivirus C

Organism

EC Number Organism UniProt Comment Textmining
2.7.7.48 Hepacivirus C
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.7.48 nucleoside triphosphate + RNAn
-
 Hepacivirus C diphosphate + RNAn+1
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.7.48 NS5B protein
-
 Hepacivirus C
2.7.7.48 RNA-dependent RNA polymerase
-
 Hepacivirus C

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.7.48 0.000004
-
 wild type enzyme Hepacivirus C 2-[4-(2-[2-cyclopentyl-5-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl]-4-hydroxy-6-oxo-3,6-dihydro-2H-pyran-2-yl]ethyl)-2-fluorophenyl]-2-methylpropanenitrile
2.7.7.48 0.00002
-
 wild type enzyme Hepacivirus C 6-[2-(5-chloro-2,4-dimethoxyphenyl)ethyl]-6-cyclopentyl-3-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfanyl]-4-hydroxy-5,6-dihydro-2H-pyran-2-one
2.7.7.48 0.000036
-
 wild type enzyme Hepacivirus C 2-[2-chloro-4-(2-[2-cyclopentyl-5-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl]-4-hydroxy-6-oxo-3,6-dihydro-2H-pyran-2-yl]ethyl)phenyl]-2-methylpropanenitrile